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1. 发明申请

WO2009076434A1 INHIBITORS OF INTEGRIN VLA-4 审中-公开
标题翻译： INTEGRIN VLA-4的抑制剂
公开(公告)号：WO2009076434A1
公开(公告)日：2009-06-18
申请号：PCT/US2008/086215
申请日：2008-12-10
申请人： MOLECULAR INSIGHT PHARMACEUTICALS, INC. , ZIMMERMAN, Craig, N. , BABICH, John, W.
发明人： ZIMMERMAN, Craig, N. , BABICH, John, W.
IPC分类号： A61K51/04 , A61K51/08 , A61P35/00 , A61P35/02
CPC分类号： A61K51/088 , A61K51/0402 , A61K51/0425 , A61K51/0446 , A61K51/0478 , A61K51/0497
摘要： A complex, its stereoisomer or pharmaceutically acceptable salt has the formula (I), where:Formula (I), wherein: W is a group that is A, B, or C: R 1 is hydrogen, alkyl or alkoxy; R 2 is a bond, hydrogen or alkyl; R 3 , R 4 and R 5 are independently hydrogen, iodine, alkyl, alkoxy, hydroxyl, amino, aminoalkyl, dialkylamino, or carboxyl; X is a bond, C=O, O=C-O, or CH 2 ; Y is a bond, CH 2 , or O; m is an integer ranging from 1 to 6; n is an integer ranging from 0 to 6; Metal represents a metallic moiety comprising a radionuclide; and Chelate represents a chelating moiety that coordinates with said radionuclide to form the complex.
摘要翻译：络合物，其立体异构体或药学上可接受的盐具有式（I），其中：式（I）其中：W是A，B或C的基团：R 1是氢，烷基或烷氧基; R2是键，氢或烷基; R3，R4和R5独立地是氢，碘，烷基，烷氧基，羟基，氨基，氨基烷基，二烷基氨基或羧基; X是键，C = O，O = C-O或CH 2; Y是键，CH2或O; m为1〜6的整数; n为0〜6的整数; 金属表示包含放射性核素的金属部分; 螯合物代表与所述放射性核素配位以形成络合物的螯合部分。

2. 发明申请

WO2008058192A2 HETERODIMERS OF GLUTAMIC ACID 审中-公开
标题翻译：谷氨酸的交联剂
公开(公告)号：WO2008058192A2
公开(公告)日：2008-05-15
申请号：PCT/US2007/083934
申请日：2007-11-07
申请人： MOLECULAR INSIGHT PHARMACEUTICALS, INC. , BABICH, John, W. , ZIMMERMAN, Craig, N. , MARESCA, Kevin, P.
发明人： BABICH, John, W. , ZIMMERMAN, Craig, N. , MARESCA, Kevin, P.
IPC分类号： C09C1/00
CPC分类号： C07C275/16 , A61K39/385 , C07B59/001 , C07C275/24 , C07C275/30 , C07C311/19 , C07D213/38
摘要： Compounds of Formula (Ia), wherein R is a C 6 -C 12 substituted or unsubstituted aryl, a C 6 -C 12 substituted or unsubstituted heteroaryl, a C 1 -C 6 substituted or unsubstituted alkyl or -NR'R', Q is C(O), O, NR', S, S(O) 2 , C(O) 2 (CH2)p Y is C(O), O, NR', S, S(O) 2 , C(O) 2 (CH2)p Z is H or C 1 -C 4 alkyl, R' is H, C(O), S(O) 2 , C(O) 2 , a C 6 -C 12 substituted or unsubstituted aryl, a C 6 -C 12 substituted or unsubstituted heteroaryl or a C 1 -C 6 substituted or unsubstituted alkyl, when substituted, aryl, heteroaryl and alkyl are substituted with halogen, C 6 -C 12 heteroaryl, -NR'R' or COOZ, which have diagnostic and therapeutic properties, such as the treatment and management of prostate cancer and other diseases related to NAALADase inhibition. Radiolabels can be incorporated into the structure through a variety of prosthetic groups attached at the X amino acid side chain via a carbon or hetero atom linkage.
摘要翻译：式（Ia）的化合物，其中R是C 6 -C 12取代或未取代的芳基，C 6 -C 6 - 取代或未取代的杂芳基，C 1 -C 6 - 取代或未取代的烷基或-NR'R'，Q是C（O），O， NR'，S，S（O）2，C（O）2（CH2）p Y是C（O），O，NR'，S，S（ C（O）2（CH 2）p Z是H或C 1 -C 4烷基，烷基，R'是H，C（O），S（O）2，C（O）2 C，C 6 -C 取代或未取代的芳基，C 6 -C 12 - 取代或未取代的杂芳基或C 1 -C 6 - 当取代的芳基，杂芳基和烷基被卤素取代时，取代或未取代的烷基取代，C 6 -C 12 - 杂芳基，-NR' R'或COOZ，其具有诊断和治疗性质，例如前列腺癌的治疗和治疗以及与NAALADase抑制相关的其它疾病。可以通过碳或杂原子连接在X氨基酸侧链上连接的各种假基团将放射性标记引入结构中。

3. 发明申请

WO1997003094A1 CELL ADHESION INHIBITORS 审中-公开
标题翻译：细胞粘附抑制剂
公开(公告)号：WO1997003094A1
公开(公告)日：1997-01-30
申请号：PCT/US1996011570
申请日：1996-07-11
申请人： BIOGEN, INC. , LIN, Ko-Chung , ADAMS, Steven, P. , CASTRO, Alfredo, C. , ZIMMERMAN, Craig, N. , CUERVO, Julio, Hernan , LEE, Wen-Cherng , HAMMOND, Charles, E. , CARTER, Mary, Beth , ALMQUIST, Ronald, G. , ENSINGER, Carol, Lee
发明人： BIOGEN, INC.
IPC分类号： C07K14/78
CPC分类号： C07K5/0821 , A61K38/00 , C07K5/0202 , C07K5/021 , C07K5/06034 , C07K5/06113 , C07K5/0806 , C07K5/0808 , C07K5/0815 , C07K5/0819 , C07K5/101 , C07K5/1013 , C07K5/1016 , C07K5/1024 , C07K14/78 , Y10S514/825 , Y10S514/826 , Y10S514/863 , Y10S514/866 , Y10S514/885 , Y10S514/903 , Y10S530/868
摘要： The present invention relates to novel compounds that are useful for inhibition and prevention of cell adhesion and cell adhesion-mediated pathologies. This invention also relates to pharmaceutical formulations comprising these compounds and methods of using them for inhibition and prevention of cell adhesion and cell adhesion-mediated pathologies. The compounds and pharmaceutical composition of this inveniton can be used as therapeutic or prophylactic agents. They are particularly well-suited for treatment of many inflammatory and autoimmune diseases.
摘要翻译：本发明涉及可用于抑制和预防细胞粘附和细胞粘附介导的病理学的新型化合物。本发明还涉及包含这些化合物的药物制剂及其用于抑制和预防细胞粘附和细胞粘附介导的病理学的方法。本发明化合物和药物组合物可用作治疗或预防剂。它们特别适用于治疗许多炎性和自身免疫性疾病。

4. 发明申请

WO1996022966A1 CELL ADHESION INHIBITORS 审中-公开
标题翻译：细胞粘附抑制剂
公开(公告)号：WO1996022966A1
公开(公告)日：1996-08-01
申请号：PCT/US1996001349
申请日：1996-01-18
申请人： BIOGEN, INC. , ADAMS, Steven, P. , LIN, Ko-Chung , LEE, Wen-Cherng , CASTRO, Alfredo, C. , ZIMMERMAN, Craig, N. , HAMMOND, Charles, E. , LIAO, Yu-Sheng , CUERVO, Julio, Hernan , SINGH, Juswinder
发明人： BIOGEN, INC.
IPC分类号： C07C237/22
CPC分类号： C07D213/75 , A61K38/00 , C07C237/22 , C07C255/19 , C07C271/22 , C07C275/28 , C07C275/42 , C07C275/54 , C07C311/06 , C07C311/21 , C07C317/50 , C07C323/60 , C07C2601/02 , C07C2601/14 , C07D209/42 , C07D213/55 , C07D215/48 , C07D277/48 , C07D317/60 , C07D405/12 , C07K7/06
摘要： The present invention relates to novel compounds that are useful for inhibition and prevention of cell adhesion and cell adhesion-mediated pathologies. This invention also relates to pharmaceutical formulations comprising these compounds and methods of using them for inhibition and prevention of cell adhesion and cell adhesion-mediated pathologies. The compounds and pharmaceutical compositions of this invention can be used as therapeutic or prophylactic agents. They are particularly well-suited for treatment of many inflammatory and autoimmune diseases.
摘要翻译：本发明涉及可用于抑制和预防细胞粘附和细胞粘附介导的病理学的新型化合物。本发明还涉及包含这些化合物的药物制剂及其用于抑制和预防细胞粘附和细胞粘附介导的病理学的方法。本发明的化合物和药物组合物可用作治疗剂或预防剂。它们特别适用于治疗许多炎性和自身免疫性疾病。

5. 发明申请

WO2008058192A3 HETERODIMERS OF GLUTAMIC ACID 审中-公开
标题翻译：谷氨酸的杂二聚体
公开(公告)号：WO2008058192A3
公开(公告)日：2008-09-12
申请号：PCT/US2007083934
申请日：2007-11-07
申请人： MOLECULAR INSIGHT PHARM INC , BABICH JOHN W , ZIMMERMAN CRAIG N , MARESCA KEVIN P
发明人： BABICH JOHN W , ZIMMERMAN CRAIG N , MARESCA KEVIN P
IPC分类号： A61K51/00
CPC分类号： C07C275/16 , A61K39/385 , C07B59/001 , C07C275/24 , C07C275/30 , C07C311/19 , C07D213/38
摘要： Compounds of Formula (Ia), wherein R is a C 6 -C 12 substituted or unsubstituted aryl, a C 6 -C 12 substituted or unsubstituted heteroaryl, a C 1 -C 6 substituted or unsubstituted alkyl or -NR'R', Q is C(O), O, NR', S, S(O) 2 , C(O) 2 (CH2)p Y is C(O), O, NR', S, S(O) 2 , C(O) 2 (CH2)p Z is H or C 1 -C 4 alkyl, R' is H, C(O), S(O) 2 , C(O) 2 , a C 6 -C 12 substituted or unsubstituted aryl, a C 6 -C 12 substituted or unsubstituted heteroaryl or a C 1 -C 6 substituted or unsubstituted alkyl, when substituted, aryl, heteroaryl and alkyl are substituted with halogen, C 6 -C 12 heteroaryl, -NR'R' or COOZ, which have diagnostic and therapeutic properties, such as the treatment and management of prostate cancer and other diseases related to NAALADase inhibition. Radiolabels can be incorporated into the structure through a variety of prosthetic groups attached at the X amino acid side chain via a carbon or hetero atom linkage.
摘要翻译：式（Ia）的化合物，其中R为C 6 -C 12取代或未取代的芳基，C 6 -C 12芳基， 12取代或未取代的杂芳基，C 1 -C 6取代或未取代的烷基或-NR'R'，Q是C（O），O， NR'，S，S（O）2，C（O）2（CH 2）p Y是C（O），O，NR'，S，S O）2，C（O）2（CH 2）p Z是H或C 1 -C 4，烷基，R'是H，C（O），S（O）2，C（O）2，C≡C 取代或未取代的芳基，取代或未取代的杂芳基或C≡C≡C12取代或未取代的杂芳基或C≡C 取代或未取代的烷基，当被取代时，芳基，杂芳基和烷基被卤素，C1-C12杂芳基，-NR' R'或COOZ，其具有诊断和治疗性质，例如前列腺癌的治疗和管理以及与NAALADase抑制相关的其他疾病。放射性标记可以通过在X氨基酸侧链上通过碳或杂原子连接连接的各种假体基团结合到结构中。

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